| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
PI4KIIIβ (IC50 = 11 nM)
PI4KIIIβ (IC50: 11 nM). UCB9608 is a selective PI4KIIIβ inhibitor with selectivity over PI3KC2 α, β, and γ. PI4KIIIβ is a lipid kinase involved in the phosphoinositide signaling pathway, which plays a role in immune cell function, vesicular trafficking, and autophagy. Inhibition of PI4KIIIβ has immunosuppressive effects. |
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| ln Vitro |
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM. UCB9608 is selective for PI4KIIIβ over PI3KC2 α, β, and γ lipid kinases[1]. UCB9608 inhibits human mixed lymphocyte reaction, the IC50 is 37 nM[1].
UCB9608 potently inhibits PI4KIIIβ with an IC50 of 11 nM. It shows selectivity over PI3KC2 α, β, and γ lipid kinases. The compound's potent and selective inhibition of PI4KIIIβ makes it a valuable tool for studying the role of PI4KIIIβ in immune function, vesicular trafficking, and autophagy. In vitro studies would evaluate its effects on PI4KIIIβ enzymatic activity and downstream signaling pathways. The compound improves metabolic stability. |
| ln Vivo |
UCB9608 is a potent immunosuppressive agent. Its in vivo effects have been characterized in animal models. The compound exhibits an excellent pharmacokinetic profile and is orally active. As a PI4KIIIβ inhibitor, it modulates immune cell function, which may have applications in autoimmune diseases and transplant rejection. Detailed in vivo efficacy data in specific disease models are limited in publicly available sources.
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| Enzyme Assay |
PI4KIIIβ kinase activity assays are performed using recombinant human PI4KIIIβ enzyme and a lipid substrate (phosphatidylinositol, PI) in kinase reaction buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 0.1% Triton X-100). The reaction is initiated by addition of ATP (containing [γ-32P]ATP or fluorescently labeled ATP) and incubated at 30°C for 30-60 minutes. The product PI-4-phosphate is extracted and quantified by scintillation counting or by lipid blotting using PI-4P-specific antibodies. Test compounds are serially diluted in DMSO and added to the reaction mixture. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate.
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| Cell Assay |
Cellular PI4KIIIβ inhibition is evaluated in immune cell lines (e.g., Jurkat T cells, Raji B cells) or primary immune cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with UCB9608 at various concentrations (0.01-10 μM) for 1-24 hours. PI4KIIIβ activity in cell lysates is measured using lipid kinase assays. Phosphoinositide levels (PI4P, PI(4,5)P2) are quantified by LC-MS or using specific antibodies. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Immune cell activation markers and cytokine production are measured by flow cytometry and ELISA. Each experiment includes vehicle controls and positive controls.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of autoimmune disease (e.g., collagen-induced arthritis, experimental autoimmune encephalomyelitis) or transplant rejection models. UCB9608 is administered orally at doses typically ranging from 1-30 mg/kg/day. Disease severity is assessed using clinical scores. At study endpoint, tissues are collected for histopathological analysis and biochemical assays. Immune cell populations in blood, spleen, and lymph nodes are analyzed by flow cytometry. Pharmacokinetic parameters are assessed in parallel. Sample sizes typically range from 8-12 animals per group.
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| ADME/Pharmacokinetics |
UCB9608 is orally active and has an excellent pharmacokinetic profile. Solubility: DMSO (>25 mg/mL); DMSO 65 mg/mL. Storage: powder at -20°C for up to 3 years; 4°C for up to 2 years. Purity: typically >98%. The compound improves metabolic stability. Bioavailability and half-life data suggest favorable pharmacokinetic properties suitable for oral administration.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for UCB9608. As a PI4KIIIβ inhibitor and immunosuppressive agent, potential toxicities may include effects on immune function, gastrointestinal tract, and autophagy. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on immune function. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
UCB9608 is also known as compound 44. It is a selective and orally active PI4KIIIβ inhibitor with an IC50 of 11 nM. It shows selectivity over PI3KC2 α, β, and γ. The compound is a potent immunosuppressive agent that improves metabolic stability and exhibits an excellent pharmacokinetic profile. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C20H26N8O2
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|---|---|
| Molecular Weight |
410.4728
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| Exact Mass |
410.217
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| Elemental Analysis |
C, 58.52; H, 6.38; N, 27.30; O, 7.80
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| CAS # |
1616413-96-7
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| Related CAS # |
1616413-96-7
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| PubChem CID |
76282073
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| Appearance |
White to off-white solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
609
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@H]1CN(CCN1C2=NC(=NC3=C2C=NN3C)N)C(=O)NC4=C(C=C(C=C4)OC)C
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| InChi Key |
WRONAJQPZWDYAR-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C20H26N8O2/c1-12-9-14(30-4)5-6-16(12)23-20(29)27-7-8-28(13(2)11-27)18-15-10-22-26(3)17(15)24-19(21)25-18/h5-6,9-10,13H,7-8,11H2,1-4H3,(H,23,29)(H2,21,24,25)/t13-/m0/s1
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| Chemical Name |
(3S)-4-(6-amino-1-methyl-pyrazolo[3,4-d]pyrimidin-4-yl)-N-(4-methoxy-2-methyl-phenyl)-3-methyl-piperazine-1-carboxamide
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| Synonyms |
UCB9608; UCB 9608; UCB-9608
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 65~82 mg/mL (158.4~199.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4362 mL | 12.1812 mL | 24.3623 mL | |
| 5 mM | 0.4872 mL | 2.4362 mL | 4.8725 mL | |
| 10 mM | 0.2436 mL | 1.2181 mL | 2.4362 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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